Ribociclib is an oral small molecule cyclindependent kinase 4/6 inhibitor,which inhibits tumor progression by inhibiting the conversion of tumor cells from G1 phase to S phase.The combination ofribociclib and letrozole was approved in the United States on March 13,2017 as a treatment for HR+/HER2-advanced and metastatic breast cancer patients.Clinical results showed that the drug on advanced and metastatic tumors had a significant inhibitory effect and could extend the survival of patients without deterioration compared with using letrozole alone.The incidence of adverse drug reactions is higher,but the tolerance is better.This article focuses on pharmacodynamics,pharmacokinetic,clinical results and adverse effects of this drug.

Objective To explore the curative effect and safety of romethamine combined with dexamethasone on the postpartum hemorrhage for patients with high risk pregnancy.Methods 80 patients with high risk pregnancy were enrolled in our hospital from June 2014 to June 2016,of which patients divided into two group randomly,Group A (n =40) accepted romethamine for hemostasis treatment,and Group B (n =40) adopted romethamine combined with dexamethasone treatment.The clinical effect and hemorrhage of patients with postpartum hemorrhage were compared,and the adverse reactions were recorded and analyzed in the period of treatment.Results After treatment,the difference of total effective rate for postpartum hemorrhage from two groups was no significance.After given medicines 0.5 h respectively in delivery process,the SBP,DBP and HR of all parturient women were rising compared with before medicine administration remarkably (P ＜ 0.05),but the difference of those between two groups was no significance.Within 24 h after delivery,the hemorrhage of Group B was lower significantly than those patients in Group A (P ＜ 0.05).The difference of shock index (SI) from Group A and Group B was no significance.The incidence of nausea and vomiting in Group B was lower than those Group A significantly (P ＜ 0.05),and the case of total adverse reactions in group B was fewer significantly than those Group A (P ＜ 0.05).Conclusions The romethamine combined with dexamethasone for the postpartum hemorrhage in patients with high risk pregnancy deserved popularization in clinic,of which not only possessed remarkably clinical effect and well safety,but also controlled the postpartum hemorrhage effectively and decreased the incidence of the adverse reactions in the period of treatment.

Objective To investigate analgesic effect of ropivacaine and bupivacaine in painless childbirth and response to maternal stress.Methods The voluntary labor analgesia maternal 210 cases in The Fifth People's Hospital of Baoji City from June 2015 to December 2016 were randomly divided into A group and B group.105 cases collected during the same period to take maternal painless childbirth as the control group,A group was given ropivacaine combined with fentanyl anesthesia,B group received bupivacaine combined with fentanyl anesthesia,observe the analgesic effect and the effect on maternal stress response.Results The difference between the groups before anesthesia score VAS was not statistically significant.After anesthesia compared with before anesthesia,A group and B VAS scores were reduced,the control group increased,the difference was statistically significant (P ＜ 0.05).And VAS in A and B group was significantly lower than the control group,the difference was statistically significant (P ＜ 0.05).After evaluation,there was no statistical difference between the two groups in MBS score.1,5 min,Apgar scores were not statistically significant in the 3 groups.Compared with the 1 rain Apgar score,Apgar scores in 3 and 5 min were increased,the difference was statistically significant (P ＜ 0.05).Blood glucose levels in B group and control group were increased (P ＜ 0.05).Cortisol levels in group A and group B before anesthesia were higher than the control group (P ＜ 0.05);A~er anesthesia,cortisol levels in group B was higher than the control group,A group was lower than that in group B (P ＜ 0.05).Before anesthesia,the ratio of insulin/blood glucose in the A group and the B group was lower than that in the control group (P ＜ 0.05),and that in A group and B group afder anesthesia was higher than that in the control group,and the level of A group was lower than that of the B group (P ＜ 0.05).Conclusion maternal analgesia with patient-controlled infusion effect,and can reduce maternal stress reaction,it is worthy of recommendation.

Objective To investigate the clinical effect of fasudil in heart failure induced by chronic pneumocardial disease and the influence in serum level of NO and ET-1.Methods 100 cases of patients with heart failure induced by chronic pneumocardial disease in our hospital from September 2013 to September 2016 were selected and divided into observation group and control group,50 cases in each group.Patients in the control group were treated with conventional therapy,and in the observation group were treated with fasudil based on the conventional therapy.Compared the clinical effect,blood oxygen partial pressure (PaO2),CO2 partial pressure (PaCO2),tricuspid regurgitation speed,fight ventricular outflow tract inside diameter(RVOT),left ventricular ejection fraction (LVEF) and serum biochemical indexes (NO and ET-1) levels.Results After treatment,the total effective rate of the observation group was significantly higher than control group (P ＜ 0.05).PaO2,LVEF,serum level of NO of the two groups were significantly higher,PaCO2,tricuspid regurgitation speed,RVOT,serum level of ET-1 significantly lower than before treatment (P ＜ 0.05),and the PaO2,LVEF,serum level of NO of observation group were significantly higher,PaCO2,tricuspid regurgitation speed,RVOT,serum level of ET-1 of observation group were significantly lower than control group (P ＜ 0.05).Conclusion Fasudil had remarkable clinical effect in heart failure induced by chronic pneumocardial disease,and improve the patient's clinical symptoms,adjust the serum level of NO and ET-1.

Objective To study the effect and mechanism of Water extract from Jiangtang Decoction (WEJTD) on diabetes mellitus and diabetic nephropathy (DN) in spontaneous type 2 diabetes mellitus model KK-Ay mice.Methods Totally 50 KK-Ay mice were randomly divided into five groups:model group,metformin (positive drug,250 mg/kg) group,WEJTD low,medium and high dose (2,4,and 8 g/kg) group,with 10 C57BL/6J mice as normal group.The relative drugs were ig administered once a day for 12 weeks,and mice in control group and model group were perfused with distilled water of equal volume.After 12 weeks' oral administration,mice were put into metabolism cages,and the food-intake,water-intake and urine volume were calculated and collected.Blood were collected to detect the concentration of IL-6,ICAM-1 and TNF-α.Then mice were executed,and HE staining and PASM staining were used to check the effect of WEJTD on kidney.Western blotting and qRT-PCR were used to detect the concentration of PI3K,Akt,NF-κB,IL-6,ICAM-1 and TNF-α in kidney.Results WEJTD can alleviate the symptoms of diabetes,such as food ration,polydipsia and polyuria (P ＜ 0.05,0.01,and 0.001);Relief the pathological changes of kidney and significantly decreased glycogen deposition (P ＜ 0.001),down-regulate the increase of IL-6,ICAM-1 and TNF-α in serum and kidney (P ＜ 0.05,0.01 and 0.001),up-regulate the phosphorylation of PI3K and Akt (P ＜ 0.05,0.01,and 0.001),and inhibit the phosphorylation of NF-κB (P ＜ 0.001).Conclusion WEJTD had positive effects on kidney morphology of KK-Ay,and the underlying mechanism might be related to the regulation of PI3K-Akt and NF-κB-mediated inflammation.

Functional abdominal pain is one of the most common problems in functional gastrointestinal disorders,and it's also one of the diseases benefit most from traditional Chinese medicine (TCM) treatment.This paper illustrates some key considerations on the study design of traditional Chinese medicine intended for the treatment of FAP based on the latest treatment and evaluation guidelines,technical guidance,professional authority works as well as the latest clinical studies,and combined with experience of clinical trial design.It hopes to offer helps for research designers in this genera.

Objective To observe the effects of Ligustrazine on proliferation of human retinal vascular endothelial cells (HRCECs) induced by high glucose.Methods HRCECs cells were divided into control (saline) group,model (25 mmol/L glucose) group,ligustrazine low,medium,high concentration (50,100 and 200 mol/L) group,cultured for 48 h.Cell proliferation was detected by MTT cytotoxicity assay.Flow cytometry was used to detect cell cycle,and the expression of VEGF was detected by ELISA analysis.Results Compared with control group,HRCECs cell proliferation,cell division (M) phase ratio and supematant of VEGF concentration in model group increased significantly (P ＜ 0.05,0.01).Compared with model group,cell proliferation,M phase ratio and supematant of VEGF in Ligustrazine low,medium and high concentration groups decreased significantly (P ＜ 0.05,0.01),and showed a concentration dependence.Conclusion Ligustrazine can inhibit the expression of VEGF in HRCECs cells induced by high glucose to block cell cycle and inhibit the proliferation of HRCECs cells.

Objective To study that puerarin can prevent the renal glucose reabsorbtion process and promote urinary glucose excretion by inhibiting sodium-dependent glucose cotransporters 2 (SGLT2) to reduce plasma glucose in diabetes rats.Methods Molecular docking was carried out on puerarin and the obtained SGLT2 complexes through homology modeling method with dapagliflozin as positive control.Chinese hamster ovary (CHO) cells stably expressing human SGLT2 and [14C]-MethylD-glucopyranoside ([14C]-AMG) as the substrate were used in vitro for the transport assays and IC50 for SGLT2.The antihyperglycemic activity ofpuerarin was operated by oral glucose tolerance test (OGTT) and urinary glucose excretion (UGE) test in rats.Results Puerarin was identified as the substrate of SGLT2 through molecular docking,but the overall effect was not as strong asdapagliflozin.In vitro experiments showed that puerarin can strongly inhibit hSGLT2,the maximum effect was about 84％ with the half inhibitory concentration (IC50) of 0.40 mol/L.OGTT results showed that glucose inhibition rates of puerarin 10,30,60 and 120 mg/kg doses were 5.1％,6.5％,16％,and 22％ respectively,in a dose-dependent manner.In the UGE experiment,the urine sugar increased with the increase of puerarin dose.Compared with model group,the 30,60,and 120 mg/kg dose groups had significant difference (P ＜ 0.05 and 0.01).Conclusion Puerarin exhibited antiglycemic activity through inhibiting SGLT2 and was considered to be a new lead compound of SGLT2 inhibitors.

Objective To investigate the anti-hyperglycemic effect of the Chinese medicine ingredients such as berberine,baicalin,puerarin and liquiritin on the optimal insulin resistance (IR)-HepG2 cell model by oleic acid.It would provide the theoretical basis for the optimization of Chinese medicine prescription or anti-hyperglycemic components combination.Methods Different concentrations (0.1,0.2,0.5,and 1.0 mmol/L) of oleic acid were used to induce HepG2 cells for different time (24,36 and 48 h),the glucose consumption was measured byglucose oxidase assay,and cell viability was detected by CCK-8 assay to define the optimal inducing concentration and time for IR-HepG2 cell model.Then the cell morphological changes were detected by oil red O staining.Finally,the stability of IR-HepG2 cell model was tested.After the IR-HepG2 model was optimally established,the glucose consumption,glycogen content and cell viability were detected after 24 h administration with different concentrations of berberine,baicalin,puerarin and liquiritin by anthrone method,glycerol phosphate oxidase assay and CCK-8 assay respectively.Results The optimal oleic acid-induced concentration was 1 mmol/L and the optimal induced time was 24 h for the IR-HepG2 cell model that could keep stable more than 36 h.Comparing with IR model group,berberine,puerarin and baicalin significantly increased the glucose consumption,whereas liquiritin did not show significant change in the glucose consumption except for 1 μmol/L.Only 160 μmol/L puerarin and 1 μmol/L baicalin significantly inhibited IR-HepG2 cell viability.Moreover,berberine,puerarin,and baicalin significantly elevated the glycogen content;Liquiritin did not change glycogen content significantly.Conclusion The IR-HepG2 cell model could be stably established with 24 h treatment of 1 mmol/L oleic acid.Berberine,puerarin,and baicalin significantly increased the glucose consumption and glycogen content in the IR-HepG2 cells.The results suggest that berberine,baicalin and puerarin maybe perform different pathways of anti-hyperglycemic effects due to different incentives ofIR.

Objective To explore the effects of water extract from Jiangtang Decoction (WEJTD) on PI3K/Akt signal pathway of skeletal muscle metabolism in KK-Ay diabetic mice.Methods Totally 50 KK-Ay mice were randomly divided into five groups:model group,metformin (positive drug,250 mg/kg) group,WEJTD low,medium,and high dose (2,4,and 8 g/kg) group,with 10 C57BL/6J mice as normal group.The relative drugs were ig administered once a day for 12 weeks,and mice in control group and model group were perfused with distilled water of equal volume.After 12 weeks' oral administration,mice were executed to separate serum,serum insulin level was detected by ELISA kit method;RNA was extracted from muscle tissue by Trizol,and real-time PCR were used to detect the level of PI3K,Akt,GLUT-4,GSK-3β,GS and IRS-1 mRNA.Results WEJTD can down-regulate concentration of insulin in serum and GSK-3β mRNA in skeletal muscle (P ＜ 0.05 and 0.001),and down-regulate mRNA of PI3K,Akt,IRS-1,GLUT-4,and GS in skeletal muscle (P ＜ 0.05,0.01,and 0.001).Conclusion WEJTD decreased glycogen deposition and stimulated glucose transport in skeletal muscle through upregulation of PI3K/Akt signaling pathway.